ArticleThe Journal of biological chemistry2025
Bifunctional compounds for targeted degradation of carbonic anhydrase IX through integrin-facilitated lysosome degradation.
Article in The Journal of biological chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- Unlocking the "undruggable": current landscape and emerging frontiers in lysosomal receptor-mediated protein degradation.Drug delivery · 2026Review
- Recent progress in small molecules targeting the acidic tumor microenvironment.Journal of enzyme inhibition and medicinal chemistry · 2026Review
- TROP2-Targeting Chimeras (TRTACs) for Tumor Cell-Selective Membrane Protein Degradation and Enhanced Drug Delivery.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Extracellular and Membrane Protein: Structure, Biological Functions, Diseases, and an Emerging Modality for Drug Discovery.MedComm · 2026Review
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Authors and funding
10 authors.
Funding
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Abstract
As an important therapeutic target, carbonic anhydrase IX (CAIX) is crucial in the pH regulation of hypoxic solid tumors, thus keeping the survival of them in acidic microenvironment and promoting their proliferation, invasion, and metastasis. To degrade endogenous CAIX, three bifunctional compounds were designed according to the integrin-facilitated lysosomal degradation strategy. These compounds are composed of a CAIX-binding ligand, an integrin-recognizing ligand, connected via a linker, which could induce CAIX degradation in an integrin- and lysosome-dependent manner. Among them, Sul-L1-RGD showed the highest degradation efficacy and could inhibit the proliferation of tumor cells under hypoxic conditions, thus it has great potential to be applied in cancer drug discovery.
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